The LANCE® Ultra KinaSelect™ Ser/Thr kit is intended for selecting the optimal peptide substrate for serine and threonine (Ser/Thr) kinases. Kinase activity is measured in aLANCE® time-resolved fluorescence resonance energy transfer(TR-FRET) assay using five different ULight™-labeled peptide substrates with their corresponding europium (Eu)-labeled anti-phospho-antibodies. Substrate/antibody pairs giving the best performance can then be used for further assay development and optimization. The five ULight™-labeled peptides andEu-labeled antibodies selected for the KinaSelect kit were found to generate signal with over 80% of a panel of 184 Ser/Thr kinases.

S:B data: Confidence in proven performance of the kinase on specific substrates; no guessing

Phospho-motifs: Substrate sequences are provided

Assay options: Multiple substrates are tested so you can select the best peptide sequence and S:B for your kinase

In LANCE Ultra kinase assays, the binding of a Eu-labeled anti-phosphosubstrate antibody to the phosphorylated ULight-labeled substrate brings donor and acceptor molecules into close proximity. After irradiation of the kinase reaction at 320 or 340 nm, the energy from the Eu donor is transferred to the ULight acceptor dye, which in turn generates light at 665 nm. The intensity of the light emission is proportional to the level of ULight-substrate phosphorylation.

Application Note

Protein kinases play a major role in normal cellular functions such as cell proliferation, angiogenesis, and cell adhesion. Dysregulation of kinase activity has been shown to be associated with several human diseases including cancer, diabetes and morphological disorders. This makes kinases crucial targets for the discovery and development of new drugs.

Dysregulation of kinase activity has been shown to be associated with several human diseases including cancer, diabetes and morphological disorders. Because of their function, kinases are crucial targets for drug discovery. Analysis of the human genomehas revealed the existence ofnearly 520 genes encoding kinases.

Poster

Protein kinases play a major role in normal cellular functions such as cell proliferation, angiogenesis, and cell adhesion. Dysregulation of kinase activity has been shown to be associated with several human diseases including cancer, diabetes and morphological disorders. This makes kinases crucial targets for drug discovery. Analysis of the human genome has revealed the existence of nearly 520 genes encoding kinases.

Protein kinases are involved in the regulation of many aspects of the cellcycle, including proliferation, differentiation, secretion and apoptosis. Aberrant protein kinase expression or functioning is a cause orconsequence of many human diseases. As a result, kinases have become extremely popular for drug discovery programs and this has prompted the development of many kinase assay technologies suitable for highthrough putscreening (HTS).

Protein tyrosine kinases (PTK) are involved in the regulation of many aspects of the cell cycle, including proliferation, differentiation, secretion and apoptosis. Aberrant protein kinase expression or function is a cause or consequence of many human diseases like cancer and atherosclerosis. As a result, kinases became very important targets in drug discovery.

Of the 518 known human kinases, 90 are tyrosine (Tyr) kinases. Protein Tyr kinases play a key role in signal transduction and normal cell growth. They are also involved in numerous proliferative diseases like cancer and atherosclerosis, in addition to a number of autoimmune diseases. For these reasons, Tyr kinases are often targets for new drug discovery in many laboratories involved in basic R&D, disease and therapeutics research, and HTS.